Rosuvastatin calcium is a potent lipid-lowering drug for treating hypercholesteremia, and is known as “super-statin” internationally due to its minor side effect and being capable of reversing hardened artery blood vessels; in addition, rosuvastatin sodium is a precursor for synthesis of rosuvastatin calcium. The structural formula of rosuvastatin sodium is as represented by formula (I):

European patent EP 0521471 discloses a method for preparing rosuvastatin sodium (I) from a fully substituted pyrimidine aldehyde and a chiral C6 side chain Wittig reagent by Wittig olefination, deprotection, diastereoselective reduction, hydrolysis and salt formation.

In this method, for the side chain, an expensive 3-tert-butyldimethysilyloxyglutaric anhydride is used as a raw material to establish a (3R)-stereocenter with a stoichiometric chiral auxiliary (−)-benzyl amygdalate, and an inflammable and explosive diethylmethoxyborane is used in the carbonyl reduction step, which brings about inconvenience to the industrial production, and also gives a high cost.
Patent WO 0049014 describes a method for preparing rosuvastatin sodium (I) from a fully substituted Wittig-Horner and a chiral C6 side chain aldehydeester by a Wittig-Horner reaction, deprotection, hydrolysis and salt formation.

In the method, a large amount of highly toxic sodium cyanide and inflammable and explosive diethylmethoxyborane are used in the process of preparing the chiral C6 side chain aldehydeester. Moreover, in the Wittig-Horner procedure, the reaction must be performed at −75° C., under rigorous reaction conditions, which is disadvantageous for mass productions.
Patent WO 2004052867 discloses a method for preparing rosuvastatin sodium (I) from a fully substituted pyrimidine aldehyde and a chiral C6 cyano side chain Wittig reagent by Wittig olefination, deprotection, diastereoselective reduction, hydrolysis and salt formation.

The method has a long chiral C6 cyano side chain route, rigorous reaction conditions and a high raw material cost, lacking a practical meaning.
Patent WO 2006067456 describes a method for preparing rosuvastatin sodium (I) from a fully substituted pyrimidine bromide and a chiral C7 alkenyl ester by a palladium-catalyzed coupling reaction, deprotection, hydrolysis and salt formation.

An expensive heavy metal palladium catalyst is used in this method, with high cost, and easy residues of the heavy metal.
World patent WO 2006076845 discloses a method for preparing rosuvastatin sodium (I) from a fully substituted pyrimidine aldehyde and diethyl cyanomethylphosphonate by Horner-Wadsworth-Emmons olefination, then reduction, catalyzed asymmetric Mukaiyama-Aldol condensation, diastereoselective carbonyl reduction, hydrolysis and salt formation.

In this method, diisobutylaluminium hydride which is unavailable in China and expensive and inflammable and explosive diethylmethoxyborane are used in the two-step reduction procedure, respectively. Moreover, the reaction conditions for the preparation of a bis-enol disilyl ether are rigorous, which is not suitable for industrial production.
Chinese patent CN 102219780 discloses the preparation of rosuvastatin sodium (I) from a fully substituted pyrimidine aldehyde and a chiral C6 tetrazole sulfone ester by Julia-Kocienski olefination, aromatic nucleus nucleophilic substitution amination, deprotection and salt formation.

This method has a long reaction route for the chiral C6 tetrazole sulfone ester side chain, a high cost, and a poor atom economy; moreover, the Julia-Kocienski reaction must be performed at −60° C., the reaction condition being rigorous.